Cercosporamide
Cercosporamide is a highly potent, ATP-competitive PKC kinase inhibitor targeting to PKC1, with an IC50 of <50 nM and a Ki of <7 nM. Cercosporamide is a unique Mnk inhibitor.
For research use only. We do not sell to patients.
- CAS No.: 131436-22-1
- Formula: C16H13NO7
- Molecular Weight:331.28
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
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Pkc1 50 nM (IC50) |
Pkc1 7 nM (Ki) |
Mnk |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HeLa | IC50 |
<3 μM
Compound: CERCO
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Cytotoxicity against human HeLa cells
Cytotoxicity against human HeLa cells
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[PMID: 29853332] |
| KMS-11 | EC50 |
>10 μM
Compound: Cercosporamide
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Antiproliferative activity against luciferase expressing human KMS11 cells after 5 days by CellTiter-Glo luminescent assay
Antiproliferative activity against luciferase expressing human KMS11 cells after 5 days by CellTiter-Glo luminescent assay
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[PMID: 27002243] |
| Sf9 | IC50 |
0.044 μM
Compound: 1
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Inhibition of Candida albicans Pkc1 expressed in insect Sf9 cells by scintillation proximity assay
Inhibition of Candida albicans Pkc1 expressed in insect Sf9 cells by scintillation proximity assay
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[PMID: 19109017] |
In Vitro
Cercosporamide is a broad-spectrum natural antifungal compound, is actually a selective and highly potent fungal Pkc1 kinase inhibitor[1]. Cercosporamide, an antifungal agent that is recently shown to act as a unique Mnk inhibitor, exhibits antileukemic properties. Cercosporamide is a potent inhibitor of phosphorylation of eIF4E at Ser209 in AML cells and results in potent inhibitory effects on primitive leukemic progenitors (CFU-L) from AML patients. To determine whether Cercosporamide exhibits negative regulatory effects on cell proliferation and viability of leukemia cells, MTT assays are conducted. When U937 cells are incubated in the presence or absence of the increasing doses of Cercosporamide, a dose-dependent suppression of cell growth is found. Similar experiments with comparable results are seen when the effects of Cercosporamide on MM6 and K562 cells are examined[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 131436-22-1
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Appearance Solid
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Molecular Weight 331.28
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Formula C16H13NO7
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Color White to yellow
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SMILES
O=C(C1=C(C([C@@]23C)=C(O)C=C1O)OC2=CC(O)=C(C(C)=O)C3=O)N
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Synonyms
(-)-Cercosporamide
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Structure Classification
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Initial Source
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
DMSO : 1 mg/mL (3.02 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
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Data Sheet (281 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
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Handling Instructions (2659 KB)
References
[1]. Sussman A, et al. Discovery of Cercosporamide, a known antifungal natural product, as a selective Pkc1 kinase inhibitor through high-throughput screening. Eukaryot Cell. 2004 Aug;3(4):932-43. [Content Brief]
[2]. Altman JK, et al. Inhibition of Mnk kinase activity by Cercosporamide and suppressive effects on acute myeloid leukemia precursors. Blood. 2013 May 2;121(18):3675-81. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 3.0186 mL | 15.0930 mL | 30.1859 mL | 75.4649 mL |
Cercosporamide Related Classifications
HY-16982 Related Classifications
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